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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2016/05/20 07:21:51」(JST)

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Timolol is a non-selective beta-adrenergic receptor antagonist indicated for treating glaucoma, heart attacks, hypertension, and migraine headache.

It is on the World Health Organization's List of Essential Medicines, a list of the most important medications needed in a basic health system.^[2]

Medical uses

In its by mouth form, it is used:

to treat high blood pressure
to prevent heart attacks
to prevent migraine headaches^[3]

In its eye drop form it is used to treat open-angle and occasionally secondary glaucoma by reducing aqueous humour production through blockage of the beta receptors on the ciliary epithelium. The pharmacological mechanism by which it actually does this is still unknown. First beta-blocker approved for topical use in treatment of glaucoma in the USA (1978). With monotherapy, depresses IOP 18-34% below baseline within first few treatments. However, there are short-term escape and long-term drift effects in some patients. That is, tolerance develops. May reduce extent of diurnal IOP curve up to 50%. IOP higher during sleep. 5-10x more potent beta-blocker than propranolol. Light sensitive; preserved with 0.01% benzalkonium Cl (and also comes BAC free). Can also be used in adjunctive therapy with pilocarpine or CAIs.^[4]

A Cochrane Systematic Review compared the effect of timolol versus brimonidine in slowing the progression of open angle glaucoma in adult participants.^[5]

Side effects

The most serious possible side effects include cardiac arrhythmias and severe bronchospasms. Timolol can also lead to fainting, congestive heart failure, depression, confusion, worsening of Raynaud's syndrome and impotence.

Side effects when given in the eye include: burning sensation, red eyes, superficial punctate keratopathy, corneal numbness.

Formulations

It is available in tablet and liquid formulations.

For ophthalmic use, timolol is also available combined with other medications:

Timolol and brimonidine
Timolol and dorzolamide
Timolol and travoprost
Timolol and latanoprost

Brand names

Timolol is marketed under many trade names worldwide.^[1]

References

^ ^a ^b Drugs.com International trade names for timolol Page accessed Feb 26, 2016
^ "WHO Model List of EssentialMedicines" (PDF). World Health Organization. October 2013. Retrieved 22 April 2014.
^ Dawn A. Marcus; Philip A. Bain (27 February 2009). Effective Migraine Treatment in Pregnant and Lactating Women: A Practical Guide. シュプリンガー・ジャパン株式会社. pp. 141–. ISBN 978-1-60327-438-8. Retrieved 14 November 2010.
^ Strohmaier, K; Snyder, E; Adamsons, I (Jul 1998). "A multicenter study comparing dorzolamide and pilocarpine as adjunctive therapy to timolol: patient preference and impact on daily life". J Am Optom Assoc 69 (7): 441–51. PMID 9697378.
^ Sena DF, Lindsley K (2013). "Neuroprotection for treatment of glaucoma in adults". Cochrane Database Syst Rev 2 (2): CD006539. doi:10.1002/14651858.CD006539.pub3. PMC 3478138. PMID 20166085.

External links

Weinstock, Leonard M.; Mulvey, Dennis M.; Tull, Roger. (1976). "Synthesis of the .beta.-adrenergic blocking agent timolol from optically active precursors". The Journal of Organic Chemistry 41 (19): 3121–3124. doi:10.1021/jo00881a011. PMID 9497.

UpToDate Contents

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1. 幼児血管腫のマネージメント management of infantile hemangiomas
2. 開放隅角緑内障：治療 open angle glaucoma treatment
3. β遮断剤中毒 beta blocker poisoning
4. 成人における片頭痛の予防的治療 preventive treatment of migraine in adults
5. 閉塞隅角緑内障 angle closure glaucoma

English Journal

Crosslinked soy protein films and their application as ophthalmic drug delivery system.

González A1, Tártara LI2, Palma SD3, Alvarez Igarzabal CI4.
Materials science & engineering. C, Materials for biological applications.Mater Sci Eng C Mater Biol Appl.2015 Jun 1;51:73-9. doi: 10.1016/j.msec.2015.02.048. Epub 2015 Feb 26.
In this research, the potential of soy protein (SPI) based-films as drug delivery devices for ocular therapy was developed. Hence, crosslinked films with a natural and non-cytotoxic crosslinking agent, genipin (Gen), coated with poly(lactic acid) (PLA), were prepared. Filmogenic solutions were loade
PMID 25842110

A simple method for the subnanomolar quantitation of seven ophthalmic drugs in the rabbit eye.

Latreille PL1, Banquy X.
Analytical and bioanalytical chemistry.Anal Bioanal Chem.2015 May;407(13):3567-78. doi: 10.1007/s00216-015-8574-9. Epub 2015 Mar 8.
This study describes the development and validation of a new liquid chromatography-tandem mass spectrometry (MS/MS) method capable of simultaneous quantitation of seven ophthalmic drugs-pilocarpine, lidocaine, atropine, proparacaine, timolol, prednisolone, and triamcinolone acetonide-within regions
PMID 25749792

Evaluation of β-Blocker Gel and Effect of Dosing Volume for Topical Delivery.

Zhang Q1, Chantasart D, Li SK.
Journal of pharmaceutical sciences.J Pharm Sci.2015 May;104(5):1721-31. doi: 10.1002/jps.24390. Epub 2015 Feb 18.
Although topical administration of β-blockers is desired because of the improved therapeutic efficacy and reduced systemic adverse effects compared with systemic administration in the treatment of infantile hemangioma, the permeation of β-blockers across skin under finite dose conditions has not b
PMID 25694227

Japanese Journal

Comparison of 24 hour control with Timoptic 0.5% and Timoptic-XE 0.5% in exfoliation and primary open-angle glaucoma

KONSTAS AG
Acta Ophthalmol Scand 77, 541-543, 1999
NAID 30013448035

Related Pictures

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★リンクテーブル★

リンク元

「チモロール」

Timolol
Systematic (IUPAC) name
	(S)-1-(tert-butylamino)-3-[(4-morpholin-4-yl-1,2,5-thiadiazol-3-yl)oxy]propan-2-ol
Clinical data
Trade names	Many names worldwide
AHFS/Drugs.com	monograph
MedlinePlus	a602022
Pregnancy; category	AU: C; US: C (Risk not ruled out); ;
Routes of; administration	oral, Ophthalmic
Legal status
Legal status	℞ (Prescription only);
Pharmacokinetic data
Bioavailability	60%
Metabolism	Hepatic: 80%
Biological half-life	2.5-5 hours
Excretion	Renal
Identifiers
CAS Number	26839-75-8
ATC code	C07AA06 (WHO) S01ED01 (WHO)
PubChem	CID 33624
IUPHAR/BPS	565
DrugBank	DB00373
ChemSpider	31013
UNII	5JKY92S7BR
KEGG	D08600
ChEBI	CHEBI:9599
ChEMBL	CHEMBL499
Chemical data
Formula	C13H24N4O3S
Molar mass	316.421 g/mol
	SMILES O[C@H](COc1nsnc1N2CCOCC2)CNC(C)(C)C ;
	InChI InChI=1S/C13H24N4O3S/c1-13(2,3)14-8-10(18)9-20-12-11(15-21-16-12)17-4-6-19-7-5-17/h10,14,18H,4-9H2,1-3H3/t10-/m0/s1 ; Key:BLJRIMJGRPQVNF-JTQLQIEISA-N ;
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　　[★]

英: timolol
化: マレイン酸チモロール timolol maleate
商: ブロカドレン BLOCARDEN、チマバック、Timoptic、Betimol; コソプト、ザラカム、チアブート、チモプトール、チモレート、デュオトラバ、ファルチモ、リズモン
関: 眼科用剤

β受容体遮断薬(競合阻害)

薬効薬理

チマバック点眼液0.5％

眼圧下降作用：チマバック点眼液0.5％は，家兎の正常眼圧を用いた試験系において，眼圧下降効果が認められた1）．また，家兎の実験的高眼圧モデルに対しても，眼圧上昇抑制及び下降効果が認められた1）．

チモプトールＸＥ点眼液０．２５％／チモプトールＸＥ点眼液０．５％

1. 眼圧下降作用

ウサギにおけるα-キモトリプシン惹起高眼圧及び水負荷による眼圧上昇試験において、チモロールマレイン酸塩の点眼は有意に眼圧上昇を抑制することが認められている。9)

2. β-受容体遮断作用

ラット、イヌ、ネコにチモロールマレイン酸塩を全身投与した場合、イソプレナリンにより惹起された心拍数、心筋収縮力及び心拍出量の増加は著明に抑制され、本剤のβ-受容体遮断作用はピンドロールと同程度、プロプラノロールより数倍強力である。10)、11) また、チモロールマレイン酸塩は有意の内因性交感神経刺激作用、直接心筋抑制作用、局所麻酔作用を示さない。10)、11)

作用機序